Search Results - "Jain, Rishi K"

Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation by Carson, Cheryl, Raman, Pichai, Tullai, Jennifer, Xu, Lei, Henault, Martin, Thomas, Emily, Yeola, Sarita, Lao, Jianmin, McPate, Mark, Verkuyl, J Martin, Marsh, George, Sarber, Jason, Amaral, Adam, Bailey, Scott, Lubicka, Danuta, Pham, Helen, Miranda, Nicolette, Ding, Jian, Tang, Hai-Ming, Ju, Haisong, Tranter, Pamela, Ji, Nan, Krastel, Philipp, Jain, Rishi K, Schumacher, Andrew M, Loureiro, Joseph J, George, Elizabeth, Berellini, Giuliano, Ross, Nathan T, Bushell, Simon M, Erdemli, Gül, Solomon, Jonathan M

“…Englerin A is a structurally unique natural product reported to selectively inhibit growth of renal cell carcinoma cell lines. A large scale phenotypic cell…”
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Ternatin and improved synthetic variants kill cancer cells by targeting the elongation factor-1A ternary complex by Carelli, Jordan D, Sethofer, Steven G, Smith, Geoffrey A, Miller, Howard R, Simard, Jillian L, Merrick, William C, Jain, Rishi K, Ross, Nathan T, Taunton, Jack

“…Cyclic peptide natural products have evolved to exploit diverse protein targets, many of which control essential cellular processes. Inspired by a series of…”
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Examining the influence of specificity ligands and ATP-competitive ligands on the overall effectiveness of bivalent kinase inhibitors by Wong, Margaret L, Murphy, Jason, Harrington, Edmund, Gower, Carrie M, Jain, Rishi K, Schirle, Markus, Thomas, Jason R

“…Identifying selective kinase inhibitors remains a major challenge. The design of bivalent inhibitors provides a rational strategy for accessing potent and…”
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Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39 by Bassilana, Frederic, Carlson, Adam, DaSilva, Jennifer A, Grosshans, Bianka, Vidal, Solange, Beck, Valerie, Wilmeringwetter, Barbara, Llamas, Luis A, Showalter, Todd B, Rigollier, Pascal, Bourret, Aaron, Ramamurthy, Arun, Wu, Xu, Harbinski, Fred, Plonsky, Samantha, Lee, Lac, Ruffner, Heinz, Grandi, Paola, Schirle, Markus, Jenkins, Jeremy, Sailer, Andreas W, Bouwmeester, Tewis, Porter, Jeffrey A, Myer, Vic, Finan, Peter M, Tallarico, John A, Kelleher, Joseph F, Seuwen, Klaus, Jain, Rishi K, Luchansky, Sarah J

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Protein Surface Recognition by Synthetic Receptors Based on a Tetraphenylporphyrin Scaffold by Jain, Rishi K, Hamilton, Andrew D

“…Receptors based on a tetraphenylporphyrin scaffold bearing different charged and hydrophobic groups have been synthesized. The interactions of these with horse…”
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Mechanism of Resistance to the WDR5 Inhibitor in MLL-Rearranged Leukemia by Liu, Lulu, Shen, Lingling, Ding, Zhilou, He, Miao, Li, En, Tallarico, John A., Jain, Rishi K., Wang, He

“…Drug resistance is a major problem often limiting the long-term effectiveness of targeted cancer therapeutics. Resistance can be acquired through mutations or…”
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Discovery and Structure-Based Design of Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)–MYC Interaction by Ding, Jian, Liu, Lulu, Chiang, Ying-Ling, Zhao, Mengxi, Liu, Hejun, Yang, Fei, Shen, Lingling, Lin, Ying, Deng, Huiwen, Gao, Jingyan, Sage, David R., West, Laura, Llamas, Luis A., Hao, Xin, Kawatkar, Sameer, Li, En, Jain, Rishi K., Tallarico, John A., Canham, Stephen M., Wang, He

“…WDR5 is a critical chromatin cofactor of MYC. WDR5 interacts with MYC through the WBM pocket and is hypothesized to anchor MYC to chromatin through its WIN…”
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Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy by Bonazzi, Simone, d'Hennezel, Eva, Beckwith, Rohan E J, Xu, Lei, Fazal, Aleem, Magracheva, Anna, Ramesh, Radha, Cernijenko, Artiom, Antonakos, Brandon, Bhang, Hyo-Eun C, Caro, Roxana García, Cobb, Jennifer S, Ornelas, Elizabeth, Ma, Xiaolei, Wartchow, Charles A, Clifton, Matthew C, Forseth, Ry R, Fortnam, Bethany Hughes, Lu, Hongbo, Csibi, Alfredo, Tullai, Jennifer, Carbonneau, Seth, Thomsen, Noel M, Larrow, Jay, Chie-Leon, Barbara, Hainzl, Dominik, Gu, Yi, Lu, Darlene, Meyer, Matthew J, Alexander, Dylan, Kinyamu-Akunda, Jacqueline, Sabatos-Peyton, Catherine A, Dales, Natalie A, Zécri, Frédéric J, Jain, Rishi K, Shulok, Janine, Wang, Y Karen, Briner, Karin, Porter, Jeffery A, Tallarico, John A, Engelman, Jeffrey A, Dranoff, Glenn, Bradner, James E, Visser, Michael, Solomon, Jonathan M

“…Malignant tumors can evade destruction by the immune system by attracting immune-suppressive regulatory T cells (Treg) cells. The IKZF2 (Helios) transcription…”
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Discovery of Potent Small-Molecule Inhibitors of WDR5-MYC Interaction by Ding, Jian, Li, Guo, Liu, Hejun, Liu, Lulu, Lin, Ying, Gao, Jingyan, Zhou, Guoqiang, Shen, Lingling, Zhao, Mengxi, Yu, Yanyan, Guo, Weihui, Hommel, Ulrich, Ottl, Johannes, Blank, Jutta, Aubin, Nicola, Wei, Yi, He, Hu, Sage, David R., Atadja, Peter W., Li, En, Jain, Rishi K., Tallarico, John A., Canham, Stephen M., Chiang, Ying-Ling, Wang, He

“…WD repeat domain 5 (WDR5) is a member of the WD40-repeat protein family that plays a critical role in multiple processes. It is also a prominent target for…”
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Activation of human STING by a molecular glue-like compound by Li, Jie, Canham, Stephen M., Wu, Hua, Henault, Martin, Chen, Lihao, Liu, Guoxun, Chen, Yu, Yu, Gary, Miller, Howard R., Hornak, Viktor, Brittain, Scott M., Michaud, Gregory A., Tutter, Antonin, Broom, Wendy, Digan, Mary Ellen, McWhirter, Sarah M., Sivick, Kelsey E., Pham, Helen T., Chen, Christine H., Tria, George S., McKenna, Jeffery M., Schirle, Markus, Mao, Xiaohong, Nicholson, Thomas B., Wang, Yuan, Jenkins, Jeremy L., Jain, Rishi K., Tallarico, John A., Patel, Sejal J., Zheng, Lianxing, Ross, Nathan T., Cho, Charles Y., Zhang, Xuewu, Bai, Xiao-Chen, Feng, Yan

“…Stimulator of interferon genes (STING) is a dimeric transmembrane adapter protein that plays a key role in the human innate immune response to infection and…”
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Discovery of a ZIP7 inhibitor from a Notch pathway screen by Nolin, Erin, Gans, Sara, Llamas, Luis, Bandyopadhyay, Somnath, Brittain, Scott M., Bernasconi-Elias, Paula, Carter, Kyle P., Loureiro, Joseph J., Thomas, Jason R., Schirle, Markus, Yang, Yi, Guo, Ning, Roma, Guglielmo, Schuierer, Sven, Beibel, Martin, Lindeman, Alicia, Sigoillot, Frederic, Chen, Amy, Xie, Kevin X., Ho, Samuel, Reece-Hoyes, John, Weihofen, Wilhelm A., Tyskiewicz, Kayla, Hoepfner, Dominic, McDonald, Richard I., Guthrie, Nicolette, Dogra, Abhishek, Guo, Haibing, Shao, Jian, Ding, Jian, Canham, Stephen M., Boynton, Geoff, George, Elizabeth L., Kang, Zhao B., Antczak, Christophe, Porter, Jeffery A., Wallace, Owen, Tallarico, John A., Palmer, Amy E., Jenkins, Jeremy L., Jain, Rishi K., Bushell, Simon M., Fryer, Christy J.

“…The identification of activating mutations in NOTCH1 in 50% of T cell acute lymphoblastic leukemia has generated interest in elucidating how these mutations…”
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Phenotypic screen identifies calcineurin-sparing FK506 analogs as BMP potentiators for treatment of acute kidney injury by Larraufie, Marie-Hélène, Gao, Xiaolin, Xia, Xiaobo, Devine, Patrick J, Kallen, Joerg, Liu, Dong, Michaud, Gregory, Harsch, Andreas, Savage, Nik, Ding, Jian, Tan, Kian, Mihalic, Manuel, Roggo, Silvio, Canham, Stephen M, Bushell, Simon M, Krastel, Philipp, Gao, Jinhai, Izaac, Aude, Altinoglu, Erhan, Lustenberger, Philipp, Salcius, Michael, Harbinski, Fred, Williams, Eric T, Zeng, Liling, Loureiro, Joseph, Cong, Feng, Fryer, Christy J, Klickstein, Lloyd, Tallarico, John A, Jain, Rishi K, Rothman, Deborah M, Wang, Shaowen

“…Acute kidney injury (AKI) is a life-threatening disease with no known curative or preventive therapies. Data from multiple animal models and human studies have…”
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A Photoaffinity Labeling-Based Chemoproteomics Strategy for Unbiased Target Deconvolution of Small Molecule Drug Candidates by Thomas, Jason R, Brittain, Scott M, Lipps, Jennifer, Llamas, Luis, Jain, Rishi K, Schirle, Markus

“…The combination of photoaffinity labeling (PAL) and quantitative chemoproteomics enables the comprehensive, unbiased determination of protein interaction…”
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Enhancing the Small-Scale Screenable Biological Space beyond Known Chemogenomics Libraries with Gray Chemical MatterCompounds with Novel Mechanisms from High-Throughput Screening Profiles by Thomas, Jason R., Shelton, Claude, Murphy, Jason, Brittain, Scott, Bray, Mark-Anthony, Aspesi, Peter, Concannon, John, King, Frederick J., Ihry, Robert J., Ho, Daniel J., Henault, Martin, Hadjikyriacou, Andrea, Neri, Marilisa, Sigoillot, Frederic D., Pham, Helen T., Shum, Matthew, Barys, Louise, Jones, Michael D., Martin, Eric J., Blechschmidt, Anke, Rieffel, Sébastien, Troxler, Thomas J., Mapa, Felipa A., Jenkins, Jeremy L., Jain, Rishi K., Kutchukian, Peter S., Schirle, Markus, Renner, Steffen

“…Phenotypic assays have become an established approach to drug discovery. Greater disease relevance is often achieved through cellular models with increased…”
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Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39 by Bassilana, Frederic, Carlson, Adam, DaSilva, Jennifer A, Grosshans, Bianka, Vidal, Solange, Beck, Valerie, Wilmeringwetter, Barbara, Llamas, Luis A, Showalter, Todd B, Rigollier, Pascal, Bourret, Aaron, Ramamurthy, Arun, Wu, Xu, Harbinski, Fred, Plonsky, Samantha, Lee, Lac, Ruffner, Heinz, Grandi, Paola, Schirle, Markus, Jenkins, Jeremy, Sailer, Andreas W, Bouwmeester, Tewis, Porter, Jeffrey A, Myer, Vic, Finan, Peter M, Tallarico, John A, Kelleher, Joseph F, Seuwen, Klaus, Jain, Rishi K, Luchansky, Sarah J

“…A new small-molecule inhibitor of the Hedgehog signaling pathway acts independently of Smoothened (Smo). Rather than acting through Smo, which is a GPCR-like…”
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Previously Uncharacterized Vacuolar-type ATPase Binding Site Discovered from Structurally Similar Compounds with Distinct Mechanisms of Action by Wang, Andrew C, Pham, Helen T, Lipps, Jennifer M, Brittain, Scott M, Harrington, Edmund, Wang, Yuan, King, Fred J, Russ, Carsten, Pan, Xuewen, Hoepfner, Dominic, Tallarico, John, Feng, Yan, Jain, Rishi K, Schirle, Markus, Thomas, Jason R

“…Using a comprehensive chemical genetics approach, we identified a member of the lignan natural product family, HTP-013, which exhibited significant…”
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1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity by Miller-Moslin, Karen, Peukert, Stefan, Jain, Rishi K, McEwan, Michael A, Karki, Rajesh, Llamas, Luis, Yusuff, Naeem, He, Feng, Li, Yanhong, Sun, Yingchuan, Dai, Miao, Perez, Lawrence, Michael, Walter, Sheng, Tao, Lei, Huangshu, Zhang, Rui, Williams, Juliet, Bourret, Aaron, Ramamurthy, Arun, Yuan, Jing, Guo, Ribo, Matsumoto, Melissa, Vattay, Anthony, Maniara, Wieslawa, Amaral, Adam, Dorsch, Marion, Kelleher, Joseph F

“…Abnormal activation of the Hedgehog (Hh) signaling pathway has been linked to several types of human cancers, and the development of small-molecule inhibitors…”
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Conversion of a Single Polypharmacological Agent into Selective Bivalent Inhibitors of Intracellular Kinase Activity by Gower, Carrie M., Thomas, Jason R., Harrington, Edmund, Murphy, Jason, Chang, Matthew E. K., Cornella-Taracido, Ivan, Jain, Rishi K., Schirle, Markus, Maly, Dustin J.

“…Loss-of-function studies are valuable for elucidating kinase function and the validation of new drug targets. While genetic techniques, such as RNAi and…”
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Substrate Activity Screening:  A Fragment-Based Method for the Rapid Identification of Nonpeptidic Protease Inhibitors by Wood, Warren J. L, Patterson, Andrew W, Tsuruoka, Hiroyuki, Jain, Rishi K, Ellman, Jonathan A

“…A new fragment-based method for the rapid development of novel and distinct classes of nonpeptidic protease inhibitors, Substrate Activity Screening (SAS), is…”
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Identification and structure–activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway by Peukert, Stefan, Jain, Rishi K., Geisser, Adrian, Sun, Yingchuan, Zhang, Rui, Bourret, Aaron, Carlson, Adam, DaSilva, Jennifer, Ramamurthy, Arun, Kelleher, Joseph F.

“…Ortho-biphenyl carboxamides, originally prepared as inhibitors of microsomal triglyceride transfer protein (MTP) have been identified as novel inhibitors of…”
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